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Faropenem sodium synthesis method from reaction by-product

A technology of faropenem sodium and by-products, which is applied in the field of synthesis of faropenem sodium from reaction by-products, can solve the problems of low yield and high cost of faropenem sodium, achieve strong controllability, easy operation, and increase the total yield of preparation Effect

Inactive Publication Date: 2006-02-15
LUNAN PHARMA GROUP CORPORATION
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  • Abstract
  • Description
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Problems solved by technology

However, this method easily produces a certain amount (about 10-15%) of by-product III, resulting in lower yield and higher cost of faropenem sodium

Method used

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  • Faropenem sodium synthesis method from reaction by-product
  • Faropenem sodium synthesis method from reaction by-product
  • Faropenem sodium synthesis method from reaction by-product

Examples

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Embodiment 1

[0021] Example 1: Preparation of Faropenem Sodium

[0022] Add 35g of compound III to the three-neck flask, dissolve it with 400mL THF, add 60mL of 15% hydrofluoric acid, raise the temperature to 65°C and react for about 18h, after TLC monitors the reaction is complete, add 200mL of water, extract with 400mL ethyl acetate, and Wash with deionized water, 100 mL saturated sodium bicarbonate solution, 100 mL saturated sodium bisulfate solution and 100 mL saturated brine, collect the organic phase, and dry over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain the deprotected product (light yellow solid 20 g), which was dissolved in 150 mL of ether and transferred to a constant pressure funnel for the next step.

[0023] Add 12g of sodium 2-ethylhexanoate, 4g of triphenylphosphine, and 1.8g of tetrakis(triphenylphosphine)palladium to the above ether solution, and stir the reaction at 50°C. After 6 hours, a large amount of pale yellow solids are ...

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Abstract

The invention provides a process for synthesizing Faropenem from reaction by-products, which has the advantages of low cost, high yield, and easy realization of reaction conditions.

Description

technical field [0001] The present invention relates to the preparation of faropenem sodium {5R-(3R, 6R)-6-(1-hydroxyethyl)-7-oxygen 3-(tetrahydro-2-furyl)-4-sulfur-1 by reaction by-products - the method of sodium azabicyclo[3.2.0]hept-2-ene-2-carboxylate}. Background technique [0002] Faropenem Sodium (Faropenem Sodium) is 5R-(3R,6R)-6-(1-hydroxyethyl-7-oxygen 3-(tetrahydro-2-furyl)-4-thio-1-azabicyclo[ 3.2.0] The general name of sodium hept-2-ene-2-carboxylate, its structural formula is: [0003] [0004] Faropenem sodium is a β-lactam antibiotic of the penem class. It was developed by Suntory Company of Japan. It was first launched in Japan in 2000. It is the first drug of this type that is stable to β-lactamase and can be taken orally. Injectable broad-spectrum antibiotics. Like other β-lactam antibiotics, faropenem plays a bactericidal effect by inhibiting the synthesis of bacterial cell walls, and is suitable for patients with different degrees of infection. It...

Claims

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Application Information

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IPC IPC(8): C07D499/04C07D499/893
Inventor 赵志全彭立增李伟
Owner LUNAN PHARMA GROUP CORPORATION
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